• Journal of Ginseng Research
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• v.42 no.2
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• pp.133-143
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• 2018

Background: AD-2 (20(R)-dammarane-3b, 12b, 20, 25-tetrol; 25-OH-PPD) is a ginsenoside and isolated from Panax ginseng, showing anticancer activity against extensive human cancer cell lines. In this study, effects and mechanisms of 1C ((20R)-3b-O-(L-alanyl)-dammarane-12b, 20, 25-triol), a modified version of AD-2, were evaluated for its development as a novel anticancer drug. Methods: MTT assay was performed to evaluate cell cytotoxic activity. Cell cycle and levels of reactive oxygen species (ROS) were determined using flow cytometry analysis. Western blotting was employed to analyze signaling pathways. Results: 1C concentration-dependently reduces prostate cancer cell viability without affecting normal human gastric epithelial cell line-1 viability. In LNCaP prostate cancer cells, 1C triggered apoptosis via Bcl-2 family-mediated mitochondria pathway, downregulated expression of mouse double minute 2, upregulated expression of p53 and stimulated ROS production. ROS scavenger, N-acetylcysteine, can attenuate 1C-induced apoptosis. 1C also inhibited the proliferation of LNCaP cells through inhibition on $Wnt/{\beta}-catenin$ signaling pathway. Conclusion: 1C shows obvious anticancer activity based on inducing cell apoptosis by Bcl-2 family-mediated mitochondria pathway and ROS production, inhibiting $Wnt/{\beta}-catenin$ signaling pathway. These findings demonstrate that 1C may provide leads as a potential agent for cancer therapy.

• The Korea Journal of Herbology
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• v.31 no.3
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• pp.43-48
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• 2016

Objectives : The objective of this research was to investigate the antioxidant activities of stem bark of Maackia amurensis extract.Methods : Stem bark of Maackia amurensis extract were prepared using 70% methanol. Methanol extracts were fractionated to hexane, chloroform, ethyl acetate, butyl alcohol, water fractions and investigated. The antioxidant activities of fractions was evaluated by four different assays as total polyphenol contents, total flavonoid contents, DPPH(1,1-diphenyl-2-picrylhydrazyl) free-radical scavenging activity and ABTS(2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) scavenging ability.Results : The yield of methanolic extracts from stem bark of Maackia amurensis was 10.16%, whereas those of its solvent fractions (hexane, chloroform, ethyl acetate, butyl alcohol, and water) were 5.45, 11.39, 13.88, 26.07, and 40.80%, respectively. The total polyphenol contents and electron donating ability of 70% methanol extracts from stem bark of Maackia amurensis were 15.44 mg/g and 194.15 μg/mL of its IC₅₀, respectively. The 70% methanol extracts showed the highest antioxidant activity. The total polyphenol content and total flavonoid content of chloroform fractions were higher in each of 201.98 mg/g and 13.55 mg/g. The chloroform fraction showed the lowest levels of DPPH(IC₅₀, 183.95 μg/mL) and ABTS scavenging activity(IC₅₀, 10.0 μg/mL). The antioxidant activity was detected in methanol extract, chloroform fractions.Conclusions : These results indicate that 70% methanol extract and its fractions of stem bark of Maackia amurensis, especially chloroform fraction, have the properties of anti-oxidant suggesting stem bark of Maackia amurensis may be a candidate for natural and functional materials.

• Advances in Traditional Medicine
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• v.8 no.4
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• pp.339-348
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• 2008

Butea frondosa has been used traditionally as a topical formulation in the treatment of many diseases and disorders. Two compounds [BF-1 (crystalline flavonol quercetin) and BF-2 (tannin) from ethyl acetate fraction of ethanolic extract] were isolated from the bark of Butea frondosa. The stereostructures of the compounds were determined on the basis of chemical and physicochemical evidence. BF-1 and BF-2 were screened in vitro for possible antibacterial property against 112 bacteria comprising 3 genera of Gram-positive and 12 genera of Gram-negative types. It was found that both BF-1 and BF-2 exhibited inhibitory activity against several bacteria. Most of these strains were inhibited by BF-1 at $50-200\;{\mu}g/ml$, while BF-2 ($MIC_{50}$ $400\;{\mu}g/ml$) was much less active. The bacteria could be arranged in the decreasing order of sensitivity towards BF-1 in the following manner: S. aureus, Bacillus spp., Salmonella spp., Vibrio spp., Shigella spp., E. coli and Pseudomonas spp. The $MIC_{50}$ of the compound was $50\;{\mu}g/ml$ while the $MIC_{90}$ was $100\;{\mu}g/ml$. The decreasing order of sensitivity towards BF-2 was V. cholerae, Bacillus spp., S. aureus, V. parahaemolyticus, Salmonella spp. and Proteus spp. BF-1 was bactericidal in action. In vivo studies with this extract showed that it could offer statistically significant protection (p < 0.01) to mice challenged with a virulent bacterium. The inhibitory activity of Butea frondosa against Gram-positive and Gram-negative bacteria indicates its usefulness in the treatment of common bacterial infections. The potentiality of BF-1 as an antibacterial agent may be confirmed further by pharmacological studies.

• Natural Product Sciences
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• v.13 no.1
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• pp.17-22
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• 2007

Fresh unripe whole fruits of Luffa tuberosa (Roxb.) or Momordica tuberosa (Roxb.) Cogn. (Cucurbitaceae) were evaluated for the antidiabetic and hyperlipidemic potential in streptozotocin (STZ) induced diabetic rats. Diabetes was induced by administration of intra-peritoneal injection of streptozotocin at a dose of 55 mg/kg body weight. After the induction of diabetes aqueous extract of L.tuberosa (AELT) was administered orally at doses of 250 and 500 mg/kg. body weight/day for a period of 14 days. The Fasting blood glucose (FBG) levels, serum insulin levels, changes in body weight, food and liquid intake were measured. In diabetic rats, the AELT exhibited significant reduction in blood glucose levels. Biochemical assay of plasma total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDLc), low-density lipoprotein cholesterol (LDLc), glycogen content and glucose-6-phosphatase activity in liver were assessed. Antihyperlipidemia in diabetic rats after the extract supplementation was confirmed by significant reduction in the levels of above mentioned hyperlipidemic indicators. This study focus on the efficacy of L.tuberosa fruits for the management of experimental STZ induced diabetic rats and provides the scientific basis of ancient herbal therapy and use of these fruits as vegetable.

• Journal of Pharmacopuncture
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• v.21 no.3
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• pp.177-184
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• 2018

Objectives: Auraptene, a natural citrus coumarin, found in plants of Rutaceae and Apiaceae families. In this study, we investigated the effects of auraptene on tumor migration, invasion and matrix metalloproteinase (MMP)-2 and -9 enzymes activity. Methods: The effects of auraptene on the viability of A2780 and Hela cell lines was evaluated by MTT assay. Wound healing migration assay and Boyden chamber assay were determined the effect of auraptene on migration and cell invasion, respectively. MMP-2 and MMP-9 activities were analyzed by gelatin zymography assay. Results: Auraptene reduced A2780 cell viability. The results showed that auraptene inhibited in vitro migration and invasion of both cells. Furthermore, cell invasion ability suppressed at $100{\mu}M$ auraptene in Hela cells and at 25, $50{\mu}M$ in A2780 cell line. Gelatin zymography showed that for Hela cell line, auraptene suppressed MMP-2 enzymatic activity in all concentrations and for MMP-9 at a concentration between 12.5 to $100{\mu}M$ in A2780 cell line. Conclusion: Auraptene inhibited migration and invasion of human cervical and ovarian cancer cells in vitro by possibly inhibitory effects on MMP-2 and MMP-9 activity.

• YAKHAK HOEJI
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• v.41 no.5
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• pp.615-621
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• 1997

Dehydropeptidase-I (DHP-I) was solubilized from porcine kidney by treatment with n-butanol and partially purified 19.25 fold by $(NH_4)_2SO_4$ precipitation, DEAE-Sepharose CL-6B ion exchange chromatography and Sephacryl S-300 HR chromatography with an overall yield of 19.16. DHP-I showed its optimal activity at pH 7.5 and 25$^{\circ}C$. Its activity was stable under neutral and alkaline conditions, but was disappeared under acidic condition. And DHP-I was heat-labile and its activity remained at 45$^{\circ}C$ for 3hrs. The enzyme was not inhibited by dicationic ions, while its activity was increased by $Co^{2+}$(1mM) and $Zn^{2+}$ (0.1mM). The enzyme was inhibited by EDTA and N-ethylmaleimide. The relative molecular mass of DHP-I was estimated to be approximately 100kDa by gel filtration chromatography. The $K_m$ value of DHP-I for glycyldehydrophenylalanine (GDHP) was 1.98mM. DWP20418 [(1R, 5S, 6S)-6-[1-(R)-Hydroxyethyl]-1-methyl-2-[(2S, 4S)-2-(piperazinylcarbonyl)-1-(R)-hydroxyethyl)pyrrolidine-4-thio]carbapen-2-em-3-carboxylic acid], compared with meropenem (MEPM), was rather easily hydrolized by DHP-I, while it was four times more resistant than imipenem (IPM) to DHP-I.

• Korean Journal of Pharmacognosy
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• v.53 no.1
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• pp.8-15
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• 2022

Robinia pseudoacacia L. (Leguminosae) is widely distributed in Asia, North America and Europe. The root bark has been traditionally used for hemostasis, arthritis and hypertension. Therefore, this study was conducted to identify the biological activity and the bioactive constituents of the root bark. We found that the methanol extract obtained from the root bark of R. pseudoacacia reduced the level of ROS and NO production in LPS-induced inflammation of RAW 264.7 cell line. Among the fractions, methylene chloride fraction showed the highest inhibitory activity against the inflammation. Seven constituents (1-7) were isolated from this fraction, and the chemical structures were determined to be medicarpin (1), (-)-vestitol (2), indole 3-carboxaldehyde (3), 3-acetylindole (4), liquiritigenin (5), 4(1H)-quinolone (6) and 8-methoxyononin (7). Among the isolates, medicarpin (1), (-)-vestitol (2), 3-acetylindole (4) and liquiritigenin (5) inhibited ROS and NO production in a dose-dependent manner. This is the first study to show the anti-inflammatory activity of the root bark of R. pseudoacacia, and it is suggested that the four constituents (1, 2, 4, and 5) could play a role in the biological activity.

• Natural Product Sciences
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• v.10 no.6
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• pp.277-283
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• 2004

Psammaplin A (PSA), a naturally occurring biophenolic compound has been demonstrated to deliver significant cytotoxicity to many cancer cell lines. In this article, we investigated the effect of PSA on cell cycle progression of lung cancer cells (A549). It was found that PSA could slightly perturb the cell cycle progression of A549 cells and lead to the cell cycle arrest at G2/M phase, indicating PSA might disturb the mitosis process of A549 cells. In addition, inspired by the two phenolic groups in the structure of PSA, the antioxidant activity of it has been evaluated. Although PSA was weak in scavenging the stable free radical 1,1-diphenyl-2-picrylhyrazyl (DPPH), it showed stronger ABTS radical scavenging activity than ascorbic acid in TEAC assay. Furthermore, it was found that PSA could effectively prevent DNA strand scission induced by oxidative stress. These results suggest that PSA have both cell cycle regulation and antioxidant activities. Herein, we suggest that PSA would be a very interesting and promising candidate to be developed as a multi-function drug.

• Natural Product Sciences
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• v.10 no.6
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• pp.272-276
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• 2004

During the course of our screening for bioactive metabolites from marine sponges, EZZ, the inseparable 1:1 mixture of (8E,13Z,20Z)-strobilinin and (7E,13Z,20Z)-felixinin has been found to deliver significant cytotoxicity against some cancer cell lines. In this study, the antioxidant activity of EZZ was first time evaluated by a series of antioxidant assays. It was found that EZZ was weak in scavenging the stable free radical 1,1-diphenyl-2-picrylhyrazyl (DPPH), but it was comparable to ascorbic acid in scavenging ABTS and superoxide radicals. In addition, EZZ could protect DNA from hydroxyl radical-induced strand cleavage. The findings of the present study suggest that EZZ possess certain antioxidant activity, which might help to prevent occurrence of cancer by alleviating the oxidative stress in cells.

• Bulletin of the Korean Chemical Society
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• v.32 no.2
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• pp.576-582
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• 2011

Various 2-amino-6-[3-(substituted phenyl)-5-phenyl-4,5-dihydropyrazol-1-yl]-4-(substituted phenyl)nicotinonitriles (3a-t) were designed and synthesized by clubbing two active anticonvulsant pharmacophores pyrazole and pyridine. All the synthesized compounds possessed the pharmacophoric elements essential for good anticonvulsant activity. The anticonvulsant screening was performed by maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) tests. Two compounds 3i and 3s showed significant anticonvulsant activity in both the screens with $ED_{50}$ values 17.5 mg/kg and 22.6 mg/kg respectively in MES screen and 154.1 mg/kg and 242.6 mg/kg respectively in scPTZ screen. They were also found to have no acute toxic effects in mice when tested at elevated doses.